Novel compounds

Abstract

Abstract Compounds of formula (I) and pharmaceutically acceptable salts thereof:wherein:n is 1, or 3; and m and p are independently 1 or 2 such that m + n + p 1≥4;X is NH; or O when Ar is offormula (a) and R₄ is hydrogen or when Ar is a group of formula (b);R₁, R₂ and R₃ are independently hydrogen, C_1-6 alkyl, phenyl or phenyl-C_1-6 alkyl, which phenyl moieties may be substituted by C_1-6 alkyl, C_1-6 alkoxy or halogen;Ar is a group of formula (a):wherein either R₄ is C_1-6 alkoxy and one of R₅, R₆ and R₇ is hydrogen and the other two are selected from hydrogen, halogen, CF₃, C_1-6 alkylthio, C_1-7 acyl, C_1-10 carboxylic acylamino, C_1-6alkyl S(O)n wherein n is 0,1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C_1-6 alkyl, C₃-₈ cycloalkyl, C_3-8 cycloalkyl C_1-4 alkyl or phenyl C_1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF₃, C_1-6 alkyl or C_1-6 alkoxy; or R₄ is hydrogen and R_s, R₆ and R₇ are independently selected from hydrogen, C_1-6 alkyl, hydroxy, C_1-6 alkoxy, C_1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C_1-2 alkylenedioxy and the third is hydrogen, C_1-6 alkyl, C_1-6 alkoxy or halo;or Ar is a group of formula (b):wherein Z is CH₂, 0, S or NR₉ wherein R₉ is hydrogen, C_1-6 alkyl, C_2-7 alkenyl, phenyl or phenyl C_1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF₃, C_1-6 alkoxy or C_1-6 alkyl; and Y is CH or N; or Z is CH or N and Y is NR_a or CHR_a where R_a is as defined for R₉ above;R_b is present when the COX linkage is attached at the phenyl ring, and is selected from hydrogen, halogen, CF₃, hydroxy, C_1-6 alkoxy or C_1-6 alkyl; R, is hydrogen, CF₃, C_1-6 alkyl, C_1-6 alkoxy, C_1-6 alkylthio, C_1-7 acyl, C_1-7 acylamino, C_1-6alkylsulphonytamino, N-(C_1-6alsulphonyl)-N-C_1-4 alkylamino, C_1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C_1-4 alkylamino optionally N-substituted byone or two groups selected from C_1-6 alkyl, C₃.₈ cycloalkyl, C_3-8 cycloalkyl C_1-4 alkyl, phenyl or phenyl C_1-4 alkyl groups or optionally N-disubstituted by C_4-5 polymethylene; having gastric motility enchancing activity and/or anti-emetic activity and/or 5-HT antagonist activity, a process for their preparation and their use as pharmaceuticals.

Inventors

• 👤 Francis David King
• 👤 Karen Anne Joiner

Bibliographic Details